METHOD FOR DESTROYING PENICILLIN ACTIVITY IN AN ANTIBIOTIC COMPRISING PENICILLIN

摘要

1,259,204. Purifying cephalosporin antibiotics. ELI LILLY & CO. 10 July, 1969 [10 July, 1968], No. 34874/69. Heading C2A. A method for freeing a mixture of cephalosporin and penicillin antibiotics from penicillin biological activity comprises treating the mixture with a 2-mercaptoamine of formula wherein RSP1/SP and RSP2/SP are hydrogen or C 1- C 9 alkyl, and RSP3/SP is hydrogen, -COOH or a salt thereof or COOR where R is C 1 -C 9 alkyl, at a pH of 4 to 9 and a temperature of 20-40‹ C. using a molar ratio of 2-mercaptoamine to penicillin of at least 1. The process is preferably performed in aqueous medium or in a mixed aqueous-organic medium of water with ethanol or dioxane. Preferred mercapto-amines are 2-aminoethanethiol, 2-dimethylamino-ethanethiol, cysteine or its ethyl ester, N-butylcysteine and 2-(N-hexylamino)ethanethiol. The penicillin activity is destroyed due to reaction with the mercaptoamine with opening of the #-lactam ring to give an amide derivative.